Document Report Card

ID: ALA1134689

Journal: J Med Chem

Title: Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.

Authors: Pagé D, Naismith A, Schmidt R, Coupal M, Labarre M, Gosselin M, Bellemare D, Payza K, Brown W.

Abstract: The design, synthesis and pharmacological evaluation of a novel class of Dmt-Tic dipeptide analogues are described. These resulting analogues bearing different C-terminal functionalities were found to bind to the human delta receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the delta receptor. Several dipeptides also showed good binding affinities with full activation of the human kappa receptor, a novel property for those ligands.

CiteXplore: 11448220

DOI: 10.1021/jm015532k